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Assay Detail

CHEMBL861287

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]DAMGO from rat mu opioid receptor expressed in HN9.10 cells
18
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Mu-type opioid receptor (CHEMBL270)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists.
Lee YS, Agnes RS, Badghisi H, Davis P, Ma SW, Lai J, Porreca F, Hruby VJ.
J Med Chem (2006) 49 : 1773 -1780
PubMed 16509592 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.63 8.92
Ki 9 7.99 9.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL375412 2 9.29
CHEMBL412331 2 9.04
CHEMBL408889 2 8.28
CHEMBL438739 2 7.80
CHEMBL374325 2 7.70
CHEMBL405192 2 7.62
CHEMBL442483 2 7.58
CHEMBL413644 2 7.51
CHEMBL408832 2 7.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL375412 Ki = 0.51 nM 9.29
CHEMBL412331 Ki = 0.92 nM 9.04
CHEMBL375412 IC50 = 1.202 nM 8.92
CHEMBL412331 IC50 = 2.138 nM 8.67
CHEMBL408889 Ki = 5.3 nM 8.28
CHEMBL408889 IC50 = 10.96 nM 7.96
CHEMBL438739 Ki = 16.0 nM 7.80
CHEMBL374325 Ki = 20.0 nM 7.70
CHEMBL405192 Ki = 24.0 nM 7.62
CHEMBL442483 Ki = 26.0 nM 7.58
CHEMBL413644 Ki = 31.0 nM 7.51
CHEMBL438739 IC50 = 37.15 nM 7.43
CHEMBL374325 IC50 = 47.86 nM 7.32
CHEMBL405192 IC50 = 54.95 nM 7.26
CHEMBL442483 IC50 = 61.66 nM 7.21
CHEMBL413644 IC50 = 64.57 nM 7.19
CHEMBL408832 Ki = 88.0 nM 7.06
CHEMBL408832 IC50 = 194.98 nM 6.71